lornoxicam and Arthritis--Rheumatoid

Lornoxicam (chlortenoxicam), a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory and antipyretic properties, is available in oral and parenteral formulations. It is distinguished from established oxicams by a relatively short elimination half-life (3 to 5 hours), which may be advantageous from a tolerability standpoint. Data from preliminary clinical trials suggest that lornoxicam is as effective as the opioid analgesics morphine, pethidine (meperidine) and tramadol in relieving postoperative pain following gynaecological or orthopaedic surgery, and as effective as other NSAIDs after oral surgery. Lornoxicam was also as effective as other NSAIDs in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. Lornoxicam has a tolerability profile characteristic of an NSAID, with gastrointestinal disturbances being the most common adverse events. Limited clinical experience to date suggests that, as with a number of other NSAIDs, lornoxicam may provide a better-tolerated alternative or adjuvant to opioid analgesics for the management of moderate to severe pain. It has also demonstrated potential as an alternative to other NSAIDs for the management of arthritis and other painful and inflammatory conditions. These preliminary findings require confirmation in further comparative and long term studies.

Topics: Absorption; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Dosage Forms; Drug Interactions; Humans; Low Back Pain; Migraine Disorders; Osteoarthritis; Pain; Pain, Postoperative; Piroxicam; Spondylitis, Ankylosing; Tissue Distribution

To assess the long term safety and therapeutic action of lornoxicam, a new non steroidal anti-inflammatory agent, in rheumatoid arthritis.. Open trial was carried out on different dosage schedules of lornoxicam (4 or 8 mg bid and 4mg tid) administered for six to twelve months. Patients of both sexes were enrolled, with classical or definite rheumatoid arthritis according to the A.R.A. criteria.. Thirty-four patients (28 F, 6 M) were admitted, mean age (+/- SD) 53.9+/-14.2 years, mean duration of illness 9.2+/-10.7 years. Lornoxicam 8-16 mg/day showed good safety and therapeutic activity in long term treatment. Clinical improvement was limited, but progression of the disease was controlled. No adverse events were complained.. Lornoxicam presented a worth-while therapeutic action and a good tolerability in rheumatoid arthritis long term treatment.

Topics: Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Female; Humans; Male; Middle Aged; Piroxicam; Time Factors

To try clinical response to xefocam, its safety, effects on arterial pressure and heart rhythm variability in rheumatoid arthritis (RA) patients with arterial hypertension (HT).. Xefocam (lornoxicam), a new non-steroid antiinflammatory drug, was given for 12 weeks in a daily dose 12 mg/day to 44 RA patients (mean age 54.5 +/- 7.3 years). 24-h arterial pressure monitoring was made with Cardiotens-01 device.. Xefocam in a dose 12 mg/day has shown good tolerance, a high analgetic and antiinflammatory effect as indicated by a positive response of articular syndrome, a significant fall of systolic arterial pressure, decreased heart rate, better heart rhythm variability.. In hypertensive RA patients xefocam in a dose 12 mg/day proved effective and safe.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antihypertensive Agents; Arthritis, Rheumatoid; Blood Pressure; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase Inhibitors; Female; Heart Rate; Humans; Hypertension; Isoenzymes; Male; Membrane Proteins; Periodicity; Piroxicam; Prostaglandin-Endoperoxide Synthases

Three studies reported here have confirmed that lornoxicam is effective in osteoarthritis and the ideal dose appears to be 12 mg daily. Overall, lornoxicam appears to be a useful drug in the treatment of both osteo- and rheumatoid arthritis, from the data presently available.

Topics: Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Double-Blind Method; Female; Humans; Male; Middle Aged; Osteoarthritis; Piroxicam

Rheumatoid arthritis (RA) is a chronic inflammatory disease treated by nonsteroidal anti-inflammatory drugs (NSAIDs) including lornoxicam (LX). Nanocarriers have been used to increase the efficacy and reduce the side effects of various drugs. The objective of the present study was to compare the therapeutic efficacy of systemic administration of lornoxicam-loaded nanomicellar formula (LX-NM) with that of free LX.. The LX-loaded mixed polymeric nanomicellar formula was prepared by direct equilibrium technique. Two rat models were used in the study: carrageenan-induced acute edema and Freund's complete adjuvant (FCA)-induced chronic arthritis.. The inhibitory effect of LX-NM on carrageenan-induced edema was higher than free LX for the same dose (1.3 mg/kg, i.p.). LX-NM (0.325 mg/kg, i.p.) produced effects comparable to that of diclofenac, which served as a standard. In the FCA model, daily treatment with LX-NM (0.325 mg/kg, i.p.) starting on day 14 significantly reduced the percentage of edema and increased weight growth. However, the same dose of LX failed to confer any significant change. Additionally, LX-NM significantly attenuated the rise of tumor necrosis factor-α (TNF-α), interleukin-1β, prostaglandin E2, nuclear factor-κβ, malondialdehyde and nitric oxide serum levels. In contrast, LX failed to show any significant reduction in elevated serum biomarkers except for TNF-α.. LX-NM is an alternative delivery system that is simply prepared at low costs. It showed a superior therapeutic efficacy against RA compared to free LX. Thus, LX-NM can be considered as a promising candidate for treatment of RA and similar inflammatory disorders.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Experimental; Arthritis, Rheumatoid; Biomarkers; Carrageenan; Chronic Disease; Dinoprostone; Disease Models, Animal; Edema; Freund's Adjuvant; Interleukin-1beta; Male; Micelles; Nanoparticles; Piroxicam; Polymers; Rats, Wistar; Thiobarbituric Acid Reactive Substances; Tumor Necrosis Factor-alpha

To assess the safety of lornoxicam with particular focus on gastrointestinal (GI) events.. Data on adverse drug reactions (ADRs) were pooled from 60 comparative studies of lornoxicam.. A total of 6420 patients received lornoxicam, 1192 received placebo and 3770 received a comparator analgesic. ADRs were reported by 21% of lornoxicam-treated patients, with GI events the most frequent (14 vs 8% with placebo). Across 15 studies that compared lornoxicam (n = 1287) with another NSAID (n = 1010), there was a reduced risk of a GI ADR with lornoxicam (0.78 [95% CI: 0.64-0.96]; p = 0.017).. Lornoxicam was well tolerated with the type of GI events observed consistent with the known safety profile of NSAIDs.

Topics: Adult; Arthritis, Rheumatoid; Clinical Trials as Topic; Cyclooxygenase Inhibitors; Female; Gastrointestinal Diseases; Humans; Male; Middle Aged; Pain; Piroxicam; Treatment Outcome

In this present research work, we have designed a pulsincap formulation comprising mini-tablets, which to the best of our knowledge this combination has not been reported yet. We successfully combined the advantages of mini-tablets technology to meet the optimized requirements of our pulsincap formulation. Our main aim was to target lornoxicam to treat rheumatoid arthritis as per the chronotherapeutic pattern of the disease. Directly compressing method was used to prepare mini-tablets. The drug, polymers and combine mixtures of drug and polymers was evaluated for pre-formulation testing. Prepared mini-tablets were also evaluated for physicochemical, dissolution and stability studies. From FTIR and DSC evaluation, we found no interaction between the drug and polymers used. For mini-tablets, all the physico-chemical parameters were in limit. The mini-tablets of lornoxicam were filled into an insoluble body of capsule, and its opening was sealed by plugging it with a polymer. The complete capsule body after sealing with a cap was given enteric coating. Different polymers in various concentrations were used as a plug, to identify the most suitable which gives a complete lag time of 5 hours when combined with 5% CAP coating. HPMC-K100M in 30% and sodium alginate in 40% concentrations were identified as the most suitable plugs. Our optimized pulsincap formulations releases lornoxicam after a lag time of 5 hrs and maximum portion of the drug will be released in the early morning hours. It was also found to be stable for a period of 6 months as per ICH guidelines.

Topics: Administration, Oral; Alginates; Antirheumatic Agents; Arthritis, Rheumatoid; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Drug Chronotherapy; Drug Stability; Glucuronic Acid; Hexuronic Acids; Humans; Hypromellose Derivatives; Kinetics; Piroxicam; Powders; Solubility; Spectroscopy, Fourier Transform Infrared; Tablets

Patients with rheumatoid arthritis (RA) often bear joint destruction and symptomatic pain. The aim of this work is to develop a compound transdermal patch containing teriflunomide (TEF) and lornoxicam (LOX) to transport these drugs across the skin with the isochronous permeation rates for RA therapy and investigate intra-articular delivery of TEF and LOX following transdermal patches applied topically. The salts of TEF and LOX with organic amines diethylamine (DEtA), triethylamine (TEtA), diethanolamine (DEA), triethanolamine (TEA) and N-(2'-hydroxy-ethanol)-piperdine (NP) were prepared to improve the skin permeation of the parent drug. The optimized patch formulation is obtained from a 3-factor, 2-level central composite design. After topical application of the optimized compound patch to only one knee joint in rabbit, intra-articular delivery of TEF and LOX on the application site was compared with that on the non-application site. Anti-inflammatory and analgesic effects of the optimized compound patch were evaluated using the adjuvant arthritis model and the pain model induced by acetic acid, respectively. The in vitro experiment results showed that the amine salts of TEF and LOX, especially TEF-TEtA and LOX-TEtA, enhanced the skin permeation of TEF and LOX from the transdermal patch system. The optimal formulation successfully displayed isochronous permeation rates for TEF and LOX across rabbit skin, and was defined with 5% of TEF-TEtA, 10% of LOX-TEtA and 15% of azone. The in vivo study showed that TEF and LOX from transdermal patches were transferred into skin, ligament and fat pad on the application site by direct diffusion and on the non-application site by the redistribution of systemic blood supply, while local absorption of TEF and LOX in synovial fluid originated from the systemic blood supply rather than direct diffusion. In the RA rat model, the results of swelling inhibition on primary arthritis of bilateral hind paws further confirmed the above-mentioned point. The optimal formulation displayed a double response on joint inflammation and symptomatic pain. In conclusion, although transdermal administration applied topically can provide a local enhanced drug delivery for the superficial joint tissues by direct diffusion, it seemed unlikely to do that for the deeper tissue synovial fluid.

Topics: Administration, Cutaneous; Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Crotonates; Hydroxybutyrates; Male; Nitriles; Piroxicam; Rabbits; Rats; Toluidines; Transdermal Patch

To assess efficacy of intraarticular administration of lornoxicam (xefocam) in patients with rheumatoid arthritis (RA).. Xefocam was injected into the knee joints of 58 patients with RA once a week for 3 weeks in a dose 8 mg. The treatment efficacy was evaluated by changes in the severity of arthralgias, pain in the joints at palpation, circumference of the knee joints at the level of the upper edge of the patella, ultrasound and thermography of the knee joints.. Xefocam relieved arthralgia (in 44 patients at least by 30%), pain in the joints at palpation and joint circumference. Ultrasound investigation registered a significant thinning of the synovial membrane and amount of exudates.. If local steroid therapy is not definitely indicated, intraarticular administration of xefocam can be effectively used for suppression of moderate inflammation in the joints in RA patients.

Topics: Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Data Interpretation, Statistical; Female; Humans; Injections, Intra-Articular; Knee Joint; Male; Middle Aged; Piroxicam; Synovitis; Time Factors; Treatment Outcome; Ultrasonography